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MX345802B - Crystalline form of pyrimidio[6,1-a]isoquinolin-4-one compound. - Google Patents

Crystalline form of pyrimidio[6,1-a]isoquinolin-4-one compound.

Info

Publication number
MX345802B
MX345802B MX2013001533A MX2013001533A MX345802B MX 345802 B MX345802 B MX 345802B MX 2013001533 A MX2013001533 A MX 2013001533A MX 2013001533 A MX2013001533 A MX 2013001533A MX 345802 B MX345802 B MX 345802B
Authority
MX
Mexico
Prior art keywords
isoquinolin
mesitylimino
pyrimido
dihydro
oxo
Prior art date
Application number
MX2013001533A
Other languages
Spanish (es)
Other versions
MX2013001533A (en
Inventor
John Alfred Walker Michael
Michel Claude Plouvier Bertrand
S Northen Julian
Fernandes Philippe
Original Assignee
Verona Pharma Plc *
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Verona Pharma Plc * filed Critical Verona Pharma Plc *
Publication of MX2013001533A publication Critical patent/MX2013001533A/en
Publication of MX345802B publication Critical patent/MX345802B/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Otolaryngology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H -pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H -pyrimido[6,1-a]-isoquinoIin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimetlioxy-4-oxo-6,7-dihydro-2 H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern.
MX2013001533A 2010-08-09 2011-08-09 Crystalline form of pyrimidio[6,1-a]isoquinolin-4-one compound. MX345802B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37189210P 2010-08-09 2010-08-09
PCT/EP2011/063694 WO2012020016A1 (en) 2010-08-09 2011-08-09 Crystalline form of pyrimidio[6,1-a]isoquinolin-4-one compound

Publications (2)

Publication Number Publication Date
MX2013001533A MX2013001533A (en) 2013-06-07
MX345802B true MX345802B (en) 2017-02-16

Family

ID=44510951

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013001533A MX345802B (en) 2010-08-09 2011-08-09 Crystalline form of pyrimidio[6,1-a]isoquinolin-4-one compound.

Country Status (21)

Country Link
US (1) US9062047B2 (en)
EP (1) EP2603509B1 (en)
JP (1) JP2017002048A (en)
KR (1) KR101860968B1 (en)
CN (1) CN103313985B (en)
AR (1) AR082601A1 (en)
AU (1) AU2011288497B2 (en)
BR (1) BR112013003087A2 (en)
CA (1) CA2807082C (en)
DK (1) DK2603509T3 (en)
ES (1) ES2483801T3 (en)
IL (1) IL224450B (en)
MX (1) MX345802B (en)
MY (1) MY157432A (en)
PH (1) PH12013500261A1 (en)
PL (1) PL2603509T3 (en)
PT (1) PT2603509E (en)
RU (1) RU2577541C2 (en)
SI (1) SI2603509T1 (en)
TW (1) TWI516488B (en)
WO (1) WO2012020016A1 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2902403C (en) * 2013-03-15 2021-06-01 Verona Pharma Plc Pde3/pde4 inhibitor/muscarinic receptor antagonist combination
ES2682105T3 (en) * 2014-05-12 2018-09-18 Verona Pharma Plc New treatment
CN111249260B (en) 2014-09-15 2023-01-10 维罗纳制药公司 Liquid inhalation formulation comprising RPL554
GB201502260D0 (en) * 2015-02-11 2015-04-01 Verona Pharma Plc Salt of Pyrimido[6,1-A]Isoquinolin-4-one compound
GB201613054D0 (en) 2016-07-28 2016-09-14 Verona Pharma Plc New compound and process
CN112368281B (en) 2018-07-13 2022-02-18 正大天晴药业集团股份有限公司 Tricyclic compounds as dual PDE3/PDE4 inhibitors
GB2578093B (en) * 2018-10-09 2020-11-18 Verona Pharma Plc Liquid pharmaceutical composition comprising RPL554 and HFA-134A
PL4092025T3 (en) * 2020-01-15 2024-10-28 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Pharmaceutical composition of tricyclic pde3/pde4 dual inhibitor compound
US20240391916A1 (en) 2021-10-29 2024-11-28 Teva Pharmaceuticals International Gmbh Solid state forms of ensifentrine and process for preparation thereof
GB202202297D0 (en) * 2022-02-21 2022-04-06 Verona Pharma Plc Formulation production process
EP4378942A1 (en) 2022-12-02 2024-06-05 Sandoz AG Crystal form of a pde3/4 inhibitor
WO2024127413A1 (en) * 2022-12-14 2024-06-20 Cipla Limited Solid state forms of ensifentrine
US12194045B1 (en) 2023-06-26 2025-01-14 Verona Pharma Plc Particulate composition

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2081117C1 (en) * 1992-09-09 1997-06-10 Глэксо Груп Лимитед Lactam derivative of physiolocically acceptable salts or solvates
ATE250602T1 (en) 1999-03-31 2003-10-15 Vernalis Ltd PYRIMIDO(6,1-A)ISOCHINOLINONE DERIVATIVES
TW200920381A (en) * 2007-07-17 2009-05-16 Combinatorx Inc Treatments of B-cell proliferative disorders

Also Published As

Publication number Publication date
AU2011288497A1 (en) 2013-03-14
KR101860968B1 (en) 2018-05-24
WO2012020016A1 (en) 2012-02-16
BR112013003087A2 (en) 2016-07-05
CA2807082C (en) 2017-07-25
AR082601A1 (en) 2012-12-19
PT2603509E (en) 2014-08-29
JP6038788B2 (en) 2016-12-07
JP2017002048A (en) 2017-01-05
CA2807082A1 (en) 2012-02-16
US9062047B2 (en) 2015-06-23
PL2603509T3 (en) 2014-11-28
KR20140009112A (en) 2014-01-22
DK2603509T3 (en) 2014-09-08
EP2603509A1 (en) 2013-06-19
MY157432A (en) 2016-06-15
CN103313985A (en) 2013-09-18
EP2603509B1 (en) 2014-06-18
CN103313985B (en) 2016-03-02
SI2603509T1 (en) 2014-10-30
RU2577541C2 (en) 2016-03-20
PH12013500261A1 (en) 2013-03-04
RU2013110225A (en) 2014-09-20
JP2013533301A (en) 2013-08-22
ES2483801T3 (en) 2014-08-07
TW201213325A (en) 2012-04-01
IL224450B (en) 2018-01-31
TWI516488B (en) 2016-01-11
US20130225616A1 (en) 2013-08-29
MX2013001533A (en) 2013-06-07
AU2011288497B2 (en) 2016-01-21

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